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Background <p>Contezolid is a novel oxazolidinone antibiotic with potent antimicrobial activity against <i>Mycobacterium tuberculosis</i>. To date, the plasma concentration profile of contezolid and its influencing factors remain poorly characterized.</p> Methods <p>This prospective observational study included patients who were diagnosed as tuberculosis and received contezolid (800&#xa0;mg every 12&#xa0;h) between July 2024 and October 2025. All patients underwent therapeutic drug monitoring to obtain steady-state trough plasma concentrations (C<sub>min</sub>) of contezolid. Demographic characteristics and laboratory examinations were recorded. The factors associated with C<sub>min</sub> of contezolid were explored.</p> Results <p>A total of 25 patients were included in the study. The C<sub>min</sub> of contezolid ranged from 0.11&#xa0;mg/L to 18.01&#xa0;mg/L. Total bilirubin was identified as the key factor influencing the C<sub>min</sub> of contezolid while no significant associations were observed with age, sex, albumin, aspartate aminotransferase, or estimated glomerular filtration rate. Furthermore, patients were grouped by their liver function, and the result revealed that moderate hepatic impairment induced a significant increase of C<sub>min</sub> from 2.98 ± 4.19&#xa0;mg/L to 9.69 ± 4.95&#xa0;mg/L.</p> Conclusion <p>The C<sub>min</sub> of contezolid exhibits substantial interindividual variability. Close monitoring is therefore recommended in patients with hepatic impairment to guide potential dose adjustments.</p>

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Towards precision dosing of contezolid: moderate hepatic impairment increases plasma concentration of contezolid in anti-tuberculosis treatment

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年4月20日

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  • Hong Lu,
  • Manjiao Fu,
  • Qunzhi Shi,
  • Lin Liu,
  • Ying Zeng,
  • Pan Yan,
  • Pengyu Li

摘要

Background

Contezolid is a novel oxazolidinone antibiotic with potent antimicrobial activity against Mycobacterium tuberculosis. To date, the plasma concentration profile of contezolid and its influencing factors remain poorly characterized.

Methods

This prospective observational study included patients who were diagnosed as tuberculosis and received contezolid (800 mg every 12 h) between July 2024 and October 2025. All patients underwent therapeutic drug monitoring to obtain steady-state trough plasma concentrations (Cmin) of contezolid. Demographic characteristics and laboratory examinations were recorded. The factors associated with Cmin of contezolid were explored.

Results

A total of 25 patients were included in the study. The Cmin of contezolid ranged from 0.11 mg/L to 18.01 mg/L. Total bilirubin was identified as the key factor influencing the Cmin of contezolid while no significant associations were observed with age, sex, albumin, aspartate aminotransferase, or estimated glomerular filtration rate. Furthermore, patients were grouped by their liver function, and the result revealed that moderate hepatic impairment induced a significant increase of Cmin from 2.98 ± 4.19 mg/L to 9.69 ± 4.95 mg/L.

Conclusion

The Cmin of contezolid exhibits substantial interindividual variability. Close monitoring is therefore recommended in patients with hepatic impairment to guide potential dose adjustments.